CA2240946C - Isoxazoline, isothiazoline et pyrazoline, inhibiteurs du facteur xa - Google Patents

Isoxazoline, isothiazoline et pyrazoline, inhibiteurs du facteur xa Download PDF

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Publication number
CA2240946C
CA2240946C CA002240946A CA2240946A CA2240946C CA 2240946 C CA2240946 C CA 2240946C CA 002240946 A CA002240946 A CA 002240946A CA 2240946 A CA2240946 A CA 2240946A CA 2240946 C CA2240946 C CA 2240946C
Authority
CA
Canada
Prior art keywords
amidinophenyl
isoxazoline
aminocarbonyl
aminosulfonylphenyl
methyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CA002240946A
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English (en)
Other versions
CA2240946A1 (fr
Inventor
Mimi Lifen Quan
John Wityak
Robert Anthony Galemmo Jr.
Petrus F.W. Stouten
James Russell Pruitt
Donald J. Phillip Pinto
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Pharma Co
Original Assignee
Bristol Myers Squibb Pharma Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Pharma Co filed Critical Bristol Myers Squibb Pharma Co
Publication of CA2240946A1 publication Critical patent/CA2240946A1/fr
Application granted granted Critical
Publication of CA2240946C publication Critical patent/CA2240946C/fr
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/04—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Treatments For Attaching Organic Compounds To Fibrous Goods (AREA)
  • Photoreceptors In Electrophotography (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

L'invention porte sur des isoxazolines, des isothiazolines ainsi que des pyrazolines, inhibiteurs du facteur Xa, sur des compositions pharmaceutiques renfermant ces composés, ainsi que sur des méthodes d'utilisation (voir fig. I) de ces composés comme agents anticoagulants pour le traitement et la prévention de troubles thrombo-emboliques. Ces composés peuvent être représentés par la formule (I) dans laquelle X représente O, S ou NR15.
CA002240946A 1995-12-21 1996-12-17 Isoxazoline, isothiazoline et pyrazoline, inhibiteurs du facteur xa Expired - Fee Related CA2240946C (fr)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US950895P 1995-12-21 1995-12-21
US60/009,508 1995-12-21
US64690396A 1996-05-08 1996-05-08
US08/646,903 1996-05-08
US3066696P 1996-11-12 1996-11-12
US60/030,666 1996-11-12
PCT/US1996/020076 WO1997023212A1 (fr) 1995-12-21 1996-12-17 ISOXAZOLINE, ISOTHIAZOLINE ET PYRAZOLINE INHIBITEURS DU FACTEUR Xa

Publications (2)

Publication Number Publication Date
CA2240946A1 CA2240946A1 (fr) 1997-07-03
CA2240946C true CA2240946C (fr) 2002-09-10

Family

ID=27358875

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002240946A Expired - Fee Related CA2240946C (fr) 1995-12-21 1996-12-17 Isoxazoline, isothiazoline et pyrazoline, inhibiteurs du facteur xa

Country Status (9)

Country Link
EP (1) EP0874629B1 (fr)
JP (1) JP2001502655A (fr)
AT (1) ATE267011T1 (fr)
AU (1) AU1335897A (fr)
CA (1) CA2240946C (fr)
DE (1) DE69632548T2 (fr)
ES (1) ES2219706T3 (fr)
HR (1) HRP960597A2 (fr)
WO (1) WO1997023212A1 (fr)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
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US6153754A (en) 1995-12-21 2000-11-28 Albany Molecular Research, Inc. Process for production of piperidine derivatives
CA2293824A1 (fr) * 1997-06-19 1998-12-23 Mimi Lifen Quan Agents aromatiques a six membres amidino utiles en tant qu'inhibiteurs du facteur xa
ZA985247B (en) * 1997-06-19 1999-12-17 Du Pont Merck Pharma Guanidine mimics as factor Xa inhibitors.
US6339099B1 (en) 1997-06-20 2002-01-15 Dupont Pharmaceuticals Company Guanidine mimics as factor Xa inhibitors
EP1007037A4 (fr) 1997-06-26 2004-10-06 Lilly Co Eli Agents antithrombotiques
JP2001515887A (ja) * 1997-09-09 2001-09-25 デュポン ファーマシューティカルズ カンパニー Ｘａ因子の阻害剤としての、ベンゾイミダゾリノン類、ベンゾオキサゾリノン類、ベンゾピペラジノン類、インダノン類、およびそれらの誘導体
DE19755268A1 (de) * 1997-12-12 1999-06-17 Merck Patent Gmbh Benzamidinderivate
WO1999041231A1 (fr) * 1998-02-17 1999-08-19 Ono Pharmaceutical Co., Ltd. Derives amidino utilises comme ingredients actifs et medicaments les contenant
EP1064270B1 (fr) 1998-03-27 2004-10-06 Bristol-Myers Squibb Pharma Company Pyrazolines et triazolines disubstituees, utilisees en tant qu'inhibiteurs du facteur xa
DE69921994T2 (de) * 1998-05-02 2005-12-01 Astrazeneca Ab Heterozyklische verbindungen mit faktor xa hemmender wirkung
GB9809349D0 (en) 1998-05-02 1998-07-01 Zeneca Ltd Heterocyclic derivatives
JP2002527438A (ja) * 1998-10-09 2002-08-27 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ４，５−ジヒドロ−イソオキサゾール誘導体及びそれらの製薬学的使用
US6319937B1 (en) * 1998-11-18 2001-11-20 Dupont Pharmaceuticals Company Isoxazoline fibrinogen receptor antagonists
AU3127900A (en) 1998-12-23 2000-07-31 Du Pont Pharmaceuticals Company Thrombin or factor xa inhibitors
JP2003502314A (ja) 1999-06-14 2003-01-21 イーライ・リリー・アンド・カンパニー 化合物
KR20030011268A (ko) 1999-07-16 2003-02-07 브리스톨-마이어스 스퀴브 파마 컴퍼니 Ｘａ 인자 억제제로서의 질소 함유 헤테로바이사이클
GB9928568D0 (en) * 1999-12-03 2000-02-02 Zeneca Ltd Chemical compounds
GB0009803D0 (en) 2000-04-25 2000-06-07 Astrazeneca Ab Chemical compounds
CA2409762A1 (fr) 2000-06-23 2002-01-03 Donald J.P. Pinto Inhibiteurs du facteur xa a substitution heteroaryl-phenyle
CN1439008A (zh) * 2000-06-23 2003-08-27 布里斯托尔-迈尔斯斯奎布药品公司 作为因子xa抑制剂的1－(杂芳环基－苯基)－稠合吡唑衍生物
WO2002000651A2 (fr) * 2000-06-27 2002-01-03 Bristol-Myers Squibb Pharma Company Inhibiteurs du facteur xa
US6586418B2 (en) 2000-06-29 2003-07-01 Bristol-Myers Squibb Company Thrombin or factor Xa inhibitors
DE10129725A1 (de) 2001-06-20 2003-01-02 Bayer Ag Kombinationstherapie substituierter Oxazolidinone
EP1443930A1 (fr) 2001-10-25 2004-08-11 AstraZeneca AB Derives d'isoxazoline utilises en tant qu'agents antimicrobiens
PA8557501A1 (es) 2001-11-12 2003-06-30 Pfizer Prod Inc Benzamida, heteroarilamida y amidas inversas
WO2003042190A1 (fr) 2001-11-12 2003-05-22 Pfizer Products Inc. Derives de n-adamantylalkyle benzamide en tant qu'antagonistes du recepteur p2x7
DK1569912T3 (en) 2002-12-03 2015-06-29 Pharmacyclics Inc 2- (2-hydroxybiphenyl-3-yl) -1h-benzoimidazole-5-carboxamidine derivatives as factor VIIa inhibitors.
PA8591801A1 (es) 2002-12-31 2004-07-26 Pfizer Prod Inc Inhibidores benzamidicos del receptor p2x7.
DK1731512T3 (en) 2004-03-05 2015-01-05 Nissan Chemical Ind Ltd Isoxazoline-substituted benzamide AND INSTRUMENTS FOR COMBATING HARMFUL ORGANISMS
JP5184891B2 (ja) 2005-01-07 2013-04-17 シンタ ファーマシューティカルズ コーポレーション 炎症及び免疫に関連する用途に用いる化合物
ES2443690T3 (es) 2005-09-02 2014-02-20 Nissan Chemical Industries, Ltd. Compuesto de benzamida sustituido con isoxazolina y agente controlador de organismos dañinos
PL1997813T3 (pl) 2006-03-10 2010-10-29 Nissan Chemical Ind Ltd Podstawiony związek izoksazolinowy i środek zwalczający szkodniki
CN101583593A (zh) 2006-11-13 2009-11-18 辉瑞产品公司 二芳基、二吡啶基和芳基-吡啶基衍生物及其用途
US9732051B2 (en) 2011-12-23 2017-08-15 Basf Se Isothiazoline compounds for combating invertebrate pests
MX354745B (es) * 2012-09-25 2018-03-16 Bayer Cropscience Ag 3-fenilisoxazolin-5-carboxamidas 5-oxi-sustituidas y 3-fenilisoxazolin-5-tioamidas 5-oxi-sustituidas herbicidas y fungicidas.
WO2014202751A1 (fr) 2013-06-21 2014-12-24 Basf Se Procédés permettant de lutter contre les nuisibles dans le soja
CA2916833A1 (fr) * 2013-06-24 2014-12-31 Basf Se Composes isothiazoline substitues par un thiophene ou un furane comme pesticides
KR102491994B1 (ko) 2016-07-07 2023-01-25 브리스톨-마이어스 스큅 컴퍼니 Rock의 억제제로서의 스피로락탐
CN110869362A (zh) * 2017-05-12 2020-03-06 国立研究开发法人理化学研究所 A类gpcr结合性化合物改性体
RU2704967C1 (ru) * 2018-06-19 2019-11-01 Федеральное государственное бюджетное образовательное учреждение высшего образования "Ярославский государственный педагогический университет им. К.Д. Ушинского (ЯГПУ им. К.Д. Ушинского) Карбоксамидные производные изоксазолина, способ их получения и применения для лечения воспалительных заболеваний

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9110858D0 (en) * 1991-05-20 1991-07-10 Shell Int Research Herbicidal compounds
HUT74690A (en) * 1993-11-24 1997-01-28 Du Pont Merck Pharma Novel isoxazoline and isoxazole fibrinogen receptor antagonists process for producing them and pharmaceutical compositions containing them
ES2120713T3 (es) * 1993-11-24 1998-11-01 Du Pont Merck Pharma Compuestos de isoxazolinas utiles como antagonistas de receptores del fibrinogeno.

Also Published As

Publication number Publication date
EP0874629A1 (fr) 1998-11-04
EP0874629B1 (fr) 2004-05-19
DE69632548D1 (de) 2004-06-24
EP0874629A4 (fr) 1999-08-04
DE69632548T2 (de) 2005-06-02
JP2001502655A (ja) 2001-02-27
ATE267011T1 (de) 2004-06-15
HRP960597A2 (en) 1998-04-30
ES2219706T3 (es) 2004-12-01
AU1335897A (en) 1997-07-17
CA2240946A1 (fr) 1997-07-03
WO1997023212A1 (fr) 1997-07-03

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